Self-microemulsion composition of insoluble medicine

Abstract

The invention discloses a self-microemulsion composition of an insoluble medicine and without an oil phase. The composition comprises active medicines, a solvent and a surfactant, and can be adsorbed by a solid adsorbent to further obtain a solid self-microemulsion composition. The high in-vitro dissolution rate and the high in-vivo biological utilization degree of the self-microemulsion composition disclosed in the invention are maintained.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a self-microemulsion composition of poorly soluble drugs. Background technique [0002] Based on the classification system of biopharmaceuticals, APIs can be divided into four categories according to their differences in solubility and permeability. Drugs with low solubility and high permeability belong to class II of the biopharmaceutical classification, and the rate-limiting step of absorption is the low dissolution rate of the drug. Dosage form plays a decisive role in the absorption of this type of drug in the gastrointestinal tract. Traditional tablets are difficult to improve the bioavailability of this type of drug. Appropriate dosage form is the key to the successful development of this type of drug product. (Lv Yifan et al., Research on the Administration Strategy of Insoluble Drugs, World Clinical Drugs, 2009, 30(1): 41-45) [0003] Microemulsion (Micro Emul...

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Problems solved by technology

[0006] It is worth noting that the above-mentioned self-microemulsion preparations all add an oil phase, which makes the existing self-microemulsion preparations have the following disadvantages: 1) the oil has a relatively large influence on the particle size of the self-microemulsion, and it has a great influence on the determination of some drugs. There is interference; 2) many oil phases (such as castor oil, olive oil, corn oil, etc.) are easily oxidized or irritating, which makes the selection of oil phases limited; , high humidity and airtightness requirements; 4) liquid oil phase, surfactants, etc. can easily dissolve the components in the capsule shell (such as gelatin, pigments, light-proofing agents and other additives), resulting in increased impurities

[0007] Therefore, existing self-microemulsion preparations have many problems that are difficult to solve from the perspective of prescription, and the development of new self-microemulsion preparations without oil phase is a problem that needs to be solved by those skilled in the art.

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